Several methods have been developed to label compounds with ¹⁸F. However, in general these are laborious and require a multistep synthesis. A method based on the chelation of ¹⁸F-aluminum fluoride ([¹⁸F]AlF) by 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA) was developed recently. The present work was aimed to radiolabel hexavalent lactoside (NOTA-HL) by [¹⁸F]AlF method for PET imaging of asialoglycoprotein receptor (ASGPR). Methods: hexavalent lactoside was conjugated with the NOTA chelate and labeled with ¹⁸F in a one-pot method. The labeling procedure was investigated with different amounts of NOTA-HL and aluminum concentration. Radiochemical yield and radiochemical purity were determined by radio-TLC and radio-HPLC respectively. In vitro stability study of [¹⁸F]AlF-HL were carried out. PET/CT imaging of normal mice injected with [¹⁸F]AlF-NOTA-HL was performed. Results: The Radiochemical yield of [¹⁸F]AlF-NOTA-HL was higher with more precursor and optimal Al⁺ concentration. The radiochemical purity of labeled product was >95% after purified by Sep-Pak cartridge to remove unbound [¹⁸F]AlF. The radiolabeling, including purification, was performed in 30 min [¹⁸F]AlF-NOTA-HL exhibited good in vitro stability. PET studies in normal mice revealed high specific accumulation of activity in the liver. Conclusion: NOTA-HL could be labeled rapidly and efficiently with aqueous ¹⁸F using AlF method. [¹⁸F]AlF-NOTA-HL would provide another efficient approach for PET imaging of ASGPR.

已经开发出几种方法来标记¹⁸ F的化合物。但是，通常这些方法很费力，并且需要多步合成。最近开发了一种基于¹⁸ F-氟化铝（[ ¹⁸ F] AlF）与1,4,7-三氮杂环壬烷-1,4,7-三乙酸（NOTA）螯合的方法。本工作旨在通过[ ¹⁸ F] AlF方法对脱唾液酸糖蛋白受体（ASGPR）进行PET成像，以放射性标记六价乳糖苷（NOTA-HL ）。方法：将六价乳糖苷与NOTA螯合物缀合并标记¹⁸一锅法中的F。用不同数量的NOTA-HL和铝浓度研究了标记程序。放射化学产率和放射化学纯度分别通过放射TLC和放射HPLC测定。进行了[ ¹⁸ F] AlF-HL的体外稳定性研究。对注射了[ ¹⁸ F] AlF-NOTA-HL的正常小鼠进行PET / CT成像。结果：[ ¹⁸ F] AlF-NOTA-HL的放射化学收率较高，且前体含量更高且Al ⁺浓度最佳。经Sep-Pak柱纯化以除去未结合的[ ¹⁸ F] AlF后，标记产物的放射化学纯度> 95％。放射性标记（包括纯化）在30分钟内进行[ ¹⁸F] AlF-NOTA-HL表现出良好的体外稳定性。在正常小鼠中进行的PET研究表明，肝脏中有较高的活性特异性积累。结论：AlF法可以在¹⁸ F水溶液中快速高效地标记NOTA-HL 。[ ¹⁸ F] AlF-NOTA-HL将为ASGPR的PET成像提供另一种有效方法。